Πλοήγηση ανά Θέμα "Substrate Specificity"
Αποτελέσματα 1-7 από 7
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4-Arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects
(2006)In a routine screening of our small-molecule compound collection we recently identified 4-arylazo-3,5-diamino-1H-pyrazoles as a novel group of ATP antagonists with moderate potency against CDK2-cyclin E. A preliminary SAR ... -
Dietary effects of Sideritis scardica “mountain tea” on human in vivo activities of xenobiotic metabolizing enzymes in healthy subjects
(2018)Sideritis scardica (S. scardica) is an endemic plant of the Balkan Peninsula traditionally used as herbal tea for inflammation and gastric disorders. Aqueous herbal extracts may affect the activity of Phase I and II enzymes ... -
Discovery of N-Phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors
(2010)Through cell-based screening of our kinase-directed compound collection, we discovered that a subset of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amines were potent cytotoxic agents against cancer cell lines, suppressed mitotic ... -
Glycogen phosphorylase revisited: Extending the resolution of the R- And T-state structures of the free enzyme and in complex with allosteric activators
(2021)The crystal structures of free T-state and R-state glycogen phosphorylase (GP) and of R-state GP in complex with the allosteric activators IMP and AMP are reported at improved resolution. GP is a validated pharmaceutical ... -
Hypoxia-induced Changes in SUMO Conjugation Affect Transcriptional Regulation under Low Oxygen
(2019)Hypoxia occurs in pathological conditions, such as cancer, as a result of the imbalance between oxygen supply and consumption by proliferating cells. HIFs are critical molecular mediators of the physiological response to ... -
A specific phospholipase C activity regulates phosphatidylinositol levels in lung surfactant of patients with acute respiratory distress syndrome
(2010)Lung surfactant (LS) is a lipid-rich material lining the inside of the lungs. It reduces surface tension at the liquid/air interface and thus, it confers protection of the alveoli from collapsing. The surfaceactive component ... -
A unique hydrophobic cluster near the active site contributes to differences in borrelidin inhibition, among threonyl-tRNA synthetases
(2005)Borrelidin, a compound with anti-microbial and anti-angiogenic properties, is a known inhibitor of bacterial and eukaryal threonyl-tRNA synthetase (ThrRS). The inhibition mechanism of borrelidin is not well understood. ...